Metabolism of macrocyclic drugs
Metabolite Tales Blog
JULY 5, 2023
Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. A structure-based design process led to improved CNS penetration as a consequence of a transition from the acyclic crizotinib predecessor to a macrocycle. Balazs et al., Drug Hunter article, June 2023.
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